公开(公告)号：US10906919B2

公开(公告)日：2021-02-02

申请号：US16220847

申请日：2018-12-14

申请人： UCB Biopharma SRL ,  Sanofi

发明人： Teresa De Haro Garcia ,  Michael Deligny ,  Jag Paul Heer ,  Joanna Rachel Quincey ,  Mengyang Xuan ,  Zhaoning Zhu ,  Daniel Christopher Brookings ,  Mark Daniel Calmiano ,  Yves Evrard ,  Martin Clive Hutchings ,  James Andrew Johnson ,  Sophie Jadot ,  Jean Keyaerts ,  Malcolm Mac Coss ,  Matthew Duncan Selby ,  Michael Alan Shaw ,  Dominique Louis Leon Swinnen ,  Laurent Schio ,  Yann Foricher ,  Bruno Filoche-Romme

IPC分类号： C07D519/00 ,  C07F7/18 ,  C07D491/08 ,  A61K31/4184 ,  A61K31/506 ,  A61K31/55 ,  C07D487/08 ,  C07D491/18 ,  C07D495/08 ,  C07D471/18 ,  C07D487/18 ,  C07D493/18 ,  C07D495/18 ,  C07D513/18

摘要： A series of fused pentacyclic imidazole derivatives, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 6,7-dihydro-7,14-methanobenzimidazo[1,2-b][2,5]benzodiazocin-5(14H)-one derivatives and analogs thereof.

公开(公告)号：US11912721B2

公开(公告)日：2024-02-27

申请号：US17102790

申请日：2020-11-24

申请人： UCB Biopharma SRL ,  Sanofi

发明人： Teresa De Haro Garcia ,  Michael Deligny ,  Jag Paul Heer ,  Joanna Rachel Quincey ,  Mengyang Xuan ,  Zhaoning Zhu ,  Daniel Christopher Brookings ,  Mark Daniel Calmiano ,  Yves Evrard ,  Martin Clive Hutchings ,  James Andrew Johnson ,  Sophie Jadot ,  Jean Keyaerts ,  Malcolm MacCoss ,  Matthew Duncan Selby ,  Michael Alan Shaw ,  Dominique Louis Leon Swinnen ,  Laurent Schio ,  Yann Foricher ,  Bruno Filoche-Romme

IPC分类号： C07D519/00 ,  C07D491/08 ,  C07D487/08 ,  C07D491/18 ,  C07D495/08 ,  C07D471/18 ,  C07D487/18 ,  C07D493/18 ,  C07D495/18 ,  C07D513/18 ,  C07F7/18 ,  A61K31/4184 ,  A61K31/506 ,  A61K31/55

CPC分类号： C07D519/00 ,  A61K31/4184 ,  A61K31/506 ,  A61K31/55 ,  C07D471/18 ,  C07D487/08 ,  C07D487/18 ,  C07D491/08 ,  C07D491/18 ,  C07D493/18 ,  C07D495/08 ,  C07D495/18 ,  C07D513/18 ,  C07F7/1804

摘要： A series of fused pentacyclic imidazole derivatives, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 6, 7-dihydro-7, 14-methanobenzimidazo[1, 2-b][2,5]benzodiazocin-5(14H)-one derivatives and analogs thereof.

公开(公告)号：US20210155637A1

公开(公告)日：2021-05-27

申请号：US17102790

申请日：2020-11-24

申请人： UCB Biopharma SRL ,  Sanofi

发明人： Teresa De Haro Garcia ,  Michael Deligny ,  Jag Paul Heer ,  Joanna Rachel Quincey ,  Mengyang Xuan ,  Zhaoning Zhu ,  Daniel Christopher Brookings ,  Mark Daniel Calmiano ,  Yves Evrard ,  Martin Clive Hutchings ,  James Andrew Johnson ,  Sophie Jadot ,  Jean Keyaerts ,  Malcolm Mac Coss ,  Matthew Duncan Selby ,  Michael Alan Shaw ,  Dominique Louis Leon Swinnen ,  Laurent Schio ,  Yann Foricher ,  Bruno Filoche-Romme

IPC分类号： C07D519/00 ,  C07F7/18 ,  C07D491/08 ,  A61K31/4184 ,  A61K31/506 ,  A61K31/55 ,  C07D487/08 ,  C07D491/18 ,  C07D495/08 ,  C07D471/18 ,  C07D487/18 ,  C07D493/18 ,  C07D495/18 ,  C07D513/18

摘要： A series of fused pentacyclic imidazole derivatives, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 6,7-dihydro-7,14-methanobenzimidazo[1,2-b][2,5]benzodiazocin-5(14H)-one derivatives and analogs thereof.

公开(公告)号：US20230250105A1

公开(公告)日：2023-08-10

申请号：US18175030

申请日：2023-02-27

申请人： UCB Biopharma SRL ,  SANOFI

发明人： Daniel Christopher Brookings ,  Teresa De Haro Garcia ,  Yann Foricher ,  Helen Tracey Horsley ,  Martin Clive Hutchings ,  James Andrew Johnson ,  Malcolm Maccoss ,  Mengyang Xuan ,  Zhaoning Zhu

IPC分类号： C07D487/18

CPC分类号： C07D487/18 ,  C07B2200/05

摘要： A compound of formula (I) as defined herein, or a pharmaceutically acceptable salt thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

公开(公告)号：US20210252012A1

公开(公告)日：2021-08-19

申请号：US17176018

申请日：2021-02-15

申请人： UCB Biopharma SRL ,  SANOFI

发明人： Daniel Christopher Brookings ,  Teresa De Haro Garcia ,  Yann Foricher ,  Helen Tracey Horsley ,  Martin Clive Hutchings ,  James Andrew Johnson ,  Malcolm Maccoss ,  Mengyang Xuan ,  Zhaoning Zhu

IPC分类号： A61K31/55 ,  C07D487/18

摘要： A compound of formula (I) as defined herein, or a pharmaceutically acceptable salt thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

公开(公告)号：US20170305932A1

公开(公告)日：2017-10-26

申请号：US15513357

申请日：2015-10-02

申请人： UCB Biopharma SPRL ,  Sanofi

发明人： Teresa De Haro Garcia ,  Michael Deligny ,  Jag Paul Heer ,  Joanna Rachel Quincey ,  Mengyang Xuan ,  Zhaoning Zhu ,  Daniel Christopher Brookings ,  Mark Daniel Calmiano ,  Yves Evrard ,  Martin Clive Hutchings ,  James Andrew Johnson ,  Sophie Jadot ,  Jean Keyaerts ,  Malcolm Mac Coss ,  Matthew Duncan Selby ,  Michael Alan Shaw ,  Dominique Louis Leon Swinnen ,  Laurent Schio ,  Yann Foricher ,  Bruno Filoche-Romme

IPC分类号： C07D519/00 ,  C07D495/18 ,  C07D487/18 ,  C07D491/18 ,  C07F7/18 ,  C07D513/18

CPC分类号： C07D519/00 ,  A61K31/4184 ,  A61K31/506 ,  A61K31/55 ,  C07D471/18 ,  C07D487/08 ,  C07D487/18 ,  C07D491/08 ,  C07D491/18 ,  C07D493/18 ,  C07D495/08 ,  C07D495/18 ,  C07D513/18 ,  C07F7/1804

摘要： A series of fused pentacyclic imidazole derivatives, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 6,7-dihydro-7,14-methanobenzimidazo[1,2-b][2,5]benzodiazocin-5(14H)-one derivatives and analogs thereof.

公开(公告)号：US09120812B2

公开(公告)日：2015-09-01

申请号：US14374838

申请日：2013-01-25

申请人： SANOFI

发明人： Alain Braun ,  Olivier Crespin ,  Yann Foricher ,  Gilbert Marciniak ,  Nicolas Muzet ,  Eric Nicolai ,  Cecile Pascal ,  Bertrand Vivet ,  Fabrice Viviani

IPC分类号： C07D498/04 ,  C07D519/00

CPC分类号： C07D498/04 ,  C07D519/00

摘要： The invention relates to bicyclic heterocyclic derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.

摘要翻译： 本发明涉及通式（I）的双环杂环衍生物及其制备方法及其治疗用途。

公开(公告)号：US20240124408A1

公开(公告)日：2024-04-18

申请号：US18267644

申请日：2021-12-16

申请人： Sanofi

发明人： Paul Justin Mueller ,  Florian Auger ,  Guillaume Begis ,  Yann Foricher ,  Christoph Grebner ,  Stéphane Hourcade ,  Stéphanie Meyfroot ,  Sven Ruf ,  Klaus Wirth

IPC分类号： C07D305/06 ,  A61P11/04 ,  C07C235/40 ,  C07C237/12

CPC分类号： C07D305/06 ,  A61P11/04 ,  C07C235/40 ,  C07C237/12

摘要： Compounds of formula (1):




wherein R1 represents a —C(R2)(R3)—[C(R4)(R5)]m-L-R6 group or —R7; and the preparation and the therapeutic uses of the compounds of formula (1) as agonists of TRPM8 receptors, useful especially in the treatment of oropharyngeal dysphagia.

公开(公告)号：US10980814B2

公开(公告)日：2021-04-20

申请号：US16497217

申请日：2018-04-24

申请人： UCB Biopharma SRL ,  SANOFI

发明人： Daniel Christopher Brookings ,  Teresa De Haro Garcia ,  Yann Foricher ,  Helen Tracey Horsley ,  Martin Clive Hutchings ,  James Andrew Johnson ,  Malcolm Maccoss ,  Mengyang Xuan ,  Zhaoning Zhu

IPC分类号： C07D487/18 ,  A61K31/55

摘要： Disclosed herein are compounds of formula (I) and pharmaceutically acceptable salt thereof, wherein variables X, R1, R2, and R3 are defined herein. These compounds are potent modulators of human TNFα activity and, accordingly, of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

公开(公告)号：US20140378433A1

公开(公告)日：2014-12-25

申请号：US14374838

申请日：2013-01-25

申请人： SANOFI

发明人： Alain Braun ,  Olivier Crespin ,  Yann Foricher ,  Gilbert Marciniak ,  Nicolas Muzet ,  Eric Nicolai ,  Cecile Pascal ,  Bertrand Vivet ,  Fabrice Viviani

IPC分类号： C07D498/04 ,  C07D519/00

CPC分类号： C07D498/04 ,  C07D519/00

摘要： The invention relates to bicydic heterocyclic derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.

摘要翻译： 本发明涉及通式（I）的双环杂环衍生物及其制备方法及其治疗用途。